Novartis is developing buparlisib (BKM-120; NVP-BKM-120), an oral phosphoinositide 3-kinase (PI3K) inhibitor which shows pro-apoptotic and antiangiogenic activity, for the potential treatment of solid tumors, primarily advanced breast cancer.
In August 2012, a phase III combination trial was initiated for ER+/HER-advanced breast cancer in postmenopausal women refractory to aromatase inhibitor therapy. In October 2012, a phase III combination study began in ER+/HER-advanced breast cancer in postmenopausal women after progression on an mTOR inhibitor. In July 2014, phase III development was ongoing and Novartis expected to file for approval in breast cancer patients naive to mTOR inhibitors in 2015 and those previously treated with mTOR inhibitors in 2016. A phase II trial began in triple negative breast cancer in June 2012. A phase II trial in HER2-positive breast cancer in the neoadjuvant setting began in September 2013.
Buparlisib is described chemically as 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine, and has the structural formula shown as Formula 1:

Buparlisib can be prepared by several methods described in prior arts, such as patents WO2007084786, WO2012044727, and so on. But the process for preparing buparlisib in the present invention disclosed herein has not yet been published.